Inhibition of cytochrome P450 3A4 activity by schisandrol A and gomisin A isolated from Fructus Schisandrae chinensis
| Autor: | Zhi-Ling Yu, Anfernee Kai-Wing Tse, Chi-Keung Wan, Guo-Yuan Zhu, Hui Wang, David Wang Fun Fong |
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| Rok vydání: | 2010 |
| Předmět: |
Schisandra chinensis
Herb-Drug Interactions Pharmaceutical Science Dioxoles Pharmacology Lignans Cyclooctanes Inhibitory Concentration 50 chemistry.chemical_compound Drug Discovery Cytochrome P-450 CYP3A polycyclic compounds Humans heterocyclic compounds ATP Binding Cassette Transporter Subfamily B Member 1 Schisandra Cytochrome P-450 CYP3A Inhibitors biology CYP3A4 Plant Extracts Hep G2 Cells Glutathione biology.organism_classification Drug Resistance Multiple Complementary and alternative medicine chemistry Fruit Gomisin A Molecular Medicine Xenobiotic Drug metabolism |
| Zdroj: | Phytomedicine. 17:702-705 |
| ISSN: | 0944-7113 |
| DOI: | 10.1016/j.phymed.2009.12.005 |
| Popis: | We studied the effects of schisandrol A (SCH) and gomisin A (GOM), two of the main bioactive components of Fructus Schisandrae chinensis, on cytochrome P450-3A4 (CYP3A4) activity and cellular glutathione (GSH) level. In a cell-free system both SCH and GOM inhibited CYP3A4 activity with IC(50) values of 32.02 microM and 1.39 microM, respectively. SCH or GOM at concentrations up to 100 microM did not alter cellular GSH level in regular HepG2 cells and P-glycoprotein overexpressing HepG2-DR cells. Since SCH and GOM may reverse multidrug resistance (MDR) by impeding the activity of P-glycoprotein, a membrane xenobiotic exporter, SCH or GOM could affect cellular drug metabolism in addition to drug uptake. |
| Databáze: | OpenAIRE |
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